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5Z-7-Oxozeaenol Covalently Binds to MAP2K7 at Cys218 in an Unprecedented Manner

5Z-7-Oxozeaenol Covalently Binds to MAP2K7 at Cys218 in an Unprecedented Manner

Yuri Sogabe, Takashi Matsumoto, Takuma Hashimoto, Yasuyuki Kirii, Masaaki Sawa, Takayoshi Kinoshita

Bioorg Med Chem Lett. 2015 Feb 1;25(3):593-6.

PMID: 25529738

Abstract:

5Z-7-Oxozeaenol (5Z7O) is a covalent bonding inhibitor against the several protein kinases (e.g., ERK2 and TAK1) that possess a free cysteine at the gatekeeper-2 position. In addition to this cysteine, MAP2K7 has three other cysteine residues that are candidate for covalent bonding by the inhibitor 5Z7O. The crystal structure of the MAP2K7/5Z7O complex revealed that the inhibitor binds to MAP2K7 at a cysteine residue located at the end of the hinge region and not at the gatekeeper-2 residue. The structural insights into the interaction of 5Z7O with MAP2K7 should aid the development of 5Z7O derivatives with improved potency and selectivity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP253863193	5Z-7-Oxozeaenol		253863-19-3	Price

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